TARRYTOWN, N.Y.--(BUSINESS WIRE)--Jun 12, 2012 - PsychoGenics
Inc. today reported positive results from a clinical study of
eltoprazine in levodopa induced
dyskinesia (LID) in Parkinson's disease (PD) patients.
Eltoprazine met the primary objective of the study by exhibiting a
statistically significant reduction in LID at the 5 mg dose (p =
0.0007) and the 7.5 mg dose (p = 0.0467), without adversely
affecting levodopa efficacy. Eltoprazine was also well tolerated in
this study and there were no serious adverse events.

Eltoprazine is a selective 5-HT1A/1B
partial agonist. Pre-clinical data from multiple models of PD show
that eltoprazine effectively reduces LID at relatively low doses.
Chronic administration of eltoprazine for 45 days shows not only
suppression of LID and no tolerance but also protection from
development of dyskinesias. In addition, other preclinical and
clinical data support the use of eltoprazine to treat the non-motor
symptoms of PD such as cognitive impairment and depression.

In this double-blind, randomized, placebo-controlled,
dose-finding study conducted at two sites in Sweden, twenty-two
patients were given single doses of eltoprazine and placebo along
with a challenge dose of levodopa at each of the 5 treatment visits
and assessed for parkinsonian and dyskinesia symptoms over a period
of three hours post-treatment. The assessments were video-taped and
scored by two independent blinded raters.

Primary efficacy was measured using the Clinical Dyskinesia
Rating Scale (CDRS) and the Unified Parkinson's Disease Rating
Scale (UPDRS). Secondary endpoints included the Rush Dyskinesia
Rating Scale and evaluation of the patients' mood using the
Hospital Anxiety & Depression Score (HADS) and
Montgomery-Asberg Depression Rating Scale (MADRS). The trial was
partially supported by a grant from The Michael J. Fox Foundation
for Parkinson's Research.

Emer Leahy, Ph.D., President & CEO of PsychoGenics said
“The results of this trial are compelling and show that
eltoprazine has the potential to address a critical unmet need in
Parkinson's disease. We are happy to have collaborated with Dr.
Andres Bjorklund, a renowned expert in the LID field and a member
of the Scientific Advisory Board of The Michael J. Fox Foundation.
We are also very appreciative of the support from the Michael J.
Fox Foundation. With these promising positive data we now intend to
progress eltoprazine to market as quickly as possible with support
from a partner”.

“Dyskinesia is a top priority for the Foundation because
of its impact on the quality of life of people living with
Parkinson's disease,” said Todd Sherer, PhD, CEO of The
Michael J. Fox Foundation. “The results presented by
PsychoGenics and Dr. Bjorklund show early promise in finding a
potential treatment for dyskinesia, and we look forward to working
with this team to drive their program forward.”

Anders Bjorklund, MD, Ph.D., Wallenberg Neuroscience Center,
University of Lund, Sweden said “There is extensive evidence
for the role of serotonin neurons in the induction and maintenance
of LID. We have shown that 5-HT1A and 5-HT1B
agonists have a synergistic effect in suppressing LID in
preclinical models. Doses of 5-HT1A and
5-HT1B receptor agonists, which individually produced a
reduction in dyskinesia, were able to further significantly reduce
dyskinesia severity when administered in combination, without
affecting the anti-parkinsonian properties of levodopa. The results
of this clinical are encouraging and in line with the data
generated in animal models.”

About Eltoprazine and its role in dyskinesias

Serotonin neurons are known to be able to convert levodopa to
dopamine, as well as store and release dopamine in an
activity-dependent manner. In advanced patients, where the dopamine
terminals have largely degenerated, serotonin terminals are
considered a major source of dopamine release. However, serotonin
neurons lack feedback control mechanisms for the release of
dopamine, such as the D2 autoreceptor and the dopamine
transporter, which normally regulate the synaptic level of dopamine
within a physiological range. Administration of levodopa, therefore
generates high swings in synaptic dopamine, causing pulsatile
stimulation of post-synaptic dopamine receptors, and the appearance
of dyskinesia. Preclinical research has shown that removal of the
serotonin innervation or activation of pre-synaptic receptors of
the serotonin neurons by a combination of 5-HT1A and
5-HT1B receptor agonists produces a suppression of LID.
On the basis of these findings it was logical to test eltoprazine
in a LID clinical trial.

Eltoprazine is a selective 5-HT1A/1B
partial agonist. Clinical data also shows statistically significant
effects in adult ADHD patients. A study supported by the National
Institutes of Mental Health (NIMH) in Cognitive Impairment
Associated with Schizophrenia (CIAS) is ongoing.

About PsychoGenics Inc.

PsychoGenics is a preclinical contract research organization
that provides a full complement of partnered drug discovery
capabilities with a focus on psychiatric, cognitive and
neurodegenerative disorders, pain, inflammation, spinal cord and
traumatic brain injury. PsychoGenics transforms drug discovery by
combining expertise in behavioral neurobiology with the power of
bioinformatics in conjunction with proprietary, high-throughput
behavioral testing platforms that rapidly screen compound libraries
for CNS activity. PsychoGenics works with pharmaceutical and
biotechnology companies, academic institutions, and not-for-profit
research foundations to help discover treatments for major
neurological and psychiatric disorders.

As the world's largest private funder of Parkinson's research,
The Michael J. Fox Foundation is dedicated to accelerating a cure
for Parkinson's disease and improved therapies for those living
with the condition today. The Foundation pursues its goals through
an aggressively funded, highly targeted research program coupled
with active global engagement of scientists, Parkinson's patients,
business leaders, clinical trial participants, donors and
volunteers. In addition to funding more than $289 million in
research to date, the Foundation has fundamentally altered the
trajectory of progress toward a cure. Operating at the hub of
worldwide Parkinson's research, the Foundation forges
groundbreaking collaborations with industry leaders, academic
scientists and government research funders; increases the flow of
participants into Parkinson's disease clinical trials with its
online tool, Fox Trial Finder; promotes Parkinson's awareness
through high-profile advocacy, events and outreach; and coordinates
the grassroots involvement of thousands of Team Fox members around
the world. Now through December 31, 2012, all new and increased
giving to The Michael J. Fox Foundation, as well as gifts from
donors who have not given since 2010 or earlier, will be matched on
a dollar-for-dollar basis with the $50-million Brin Wojcicki
Challenge, launched by Sergey Brin and Anne Wojcicki.

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